Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine. |
Brands | Davedax Edronax Norebox Prolift Solvex Vestra
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Categories | Adrenergic Uptake Inhibitors Antidepressive Agents
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Synonyms | Reboxetine mesylate
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indication
For the treatment of clinical depression.
pharmacology
Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of new antidepressant class. Reboxetine is an a-ariloxybenzyl derivative of morpholine. Reboxetine is primarily used to treat depression but has also been found useful in the treatment of narcolepsy and panic disorders.
mechanism of action
Reboxetine is a selective inhibitor of noradrenaline reuptake. It inhibits noradrenaline reuptake
in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine. Reboxetine does not affect dopamine or serotonin reuptake and it has low
in vivo and
in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.
toxicity
Reports of seizures (rare) have been reported
biotransformation
Reboxetine is metabolized by dealkylation, hydroxylation and oxidation followed
by glucuronide or sulphate conjugation. It is metabolized by the cytochrome P450
CYP isoenzyme 3A4.
absorption
Reboxetine is rapidly and extensively absorbed following oral administration.
half life
12.5 hours